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Novel enantiopure isoxazolidine and C-alkyl imine oxide derivatives as potential hypoglycemic agents: Design, synthesis, dual inhibitors of α-amylase and α-glucosidase, ADMET and molecular docking study
New pure forms of isoxazolidine and C-alkyl imine oxide compounds as possible blood sugar-lowering agents: design, creation, dual inhibition of carbohydrate-digesting enzymes, safety, and molecular modeling
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Abstract
Compounds 7b and 7a are identified as potent inhibitors of human pancreatic α-amylase and human lysosomal acid-α-glucosidase, with inhibitory effects up to 9 and 21 times higher than acarbose, respectively.
- The newly synthesized isoxazolidine and C-alkyl imine oxide derivatives showed higher potency against human pancreatic α-amylase and human lysosomal acid-α-glucosidase compared to acarbose.
- Compound 7b demonstrated an inhibitory concentration of 23.1 ± 1.1 μM for human pancreatic α-amylase.
- Compound 7a exhibited an inhibitory concentration of 36.3 ± 1.6 μM for human lysosomal acid-α-glucosidase.
- Molecular docking studies indicated that compounds 7b and 7a may have stronger interactions with the active sites of the target enzymes.
- An in silico ADMET profile suggested satisfactory oral druglikeness and absence of toxic effects for both compounds.
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